aldehyde dehydrogenase (aldh)

Disulfiram (TETD) is an inhibitor of the acetaldehyde dehydrogenase ALDH, inhibiting hALDH1 and hALDH2 (IC50=0.15 1.45 μM) with specificity. Disulfiram is acutely sensitized to alcohol and also inhibits GSDMD pore formation.

Dyclonine hydrochloride (Dyclonine HCl) , an over the counter throat lozenge, is found in Sucretswith local anesthetic effect .

Taraxerone has allelopathic and antifungal effects.Taraxerone prevents catalase, superoxide dismutase, and reduces glutathione concentrations from the decrease induced by ethanol administration with the concentration dependent manner.

NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with an IC50 of 40 nM.

3-Hydroxybenzaldehyde is a compound useful in organic synthesis.

4-Diethylaminobenzaldehyde, a reversible aldehyde dehydrogenase (ALDH) inhibitor (Ki: 4 nM for ALDH1), exhibits a potent anti-androgenic effect (IC50: 1.71 μM).

inhibitor of aldehyde dehydrogenase 1a2 (ALDH1a2)

MeDTC (S-Methyl-N,N-diethylthiocarbamate Sulfone), a metabolite of Disulfiram, serves as a potent and irreversible inhibitor of aldehyde dehydrogenase (ALDH) [1].

1. Prunetin (Prunusetin) significantly reduces serum levels of inflammatory cytokines and mortality in mice challenged with lipopolysaccharide. 2. Prunetin mediates anti-obesity adipogenesis effects by suppressing obesity-related transcription through a feedback mechanism that regulates the expression of adiponectin, adipoR1, adipoR2, and AMPK. 3. Prunetin and biochanin A are potent reducers of NF-κB and ERK activation, zonula occludens 1 tyrosine phosphorylation, and metalloproteinase-mediated shedding activity, which may account for the barrier-improving ability of these isoflavones. 4. Prunetin significantly suppresses ATP-induced mucin secretion from cultured RTSE cells; Prunetin inhibits the production of MUC5AC mucin protein induced by EGF or PMA from NCI-H292 cells; Prunetin also inhibits the expression of MUC5AC mucin gene induced by EGF or PMA from NCI-H292 cells.

BODIPY aminoacetaldehyde (BAAA) is a fluorescent substrate for aldehyde dehydrogenase (ALDH) and can be used to isolate human hematopoietic stem cells based on ALDH activity.

CM39 is an ALDH inhibitor. Aldehyde dehydrogenase (ALDH) activity is commonly used as a marker to identify cancer stem-like cells. The three ALDH1A isoforms have all been individually implicated in cancer stem-like cells and in chemoresistance.

BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the efflux pump P-glycoprotein (P-gp) but co-application of BAAA with a P-gp inhibitor, such as verapamil , inhibits BAA efflux.2BAAA-DA has been used to isolate human hematopoietic progenitor cells, which have high ALDH activity, andviaflow cytometry to sort cancer stem cells that contain high levels of ALDH.1,3BAA used in cells can be excited at 488 nm and displays an emission maximum of 512 nm.4 1.Storms, R.W., Trujillo, A.P., Springer, J.B., et al.Isolation of primitive human hematopoietic progenitors on the basis of aldehyde dehydrogenase activityProceedings of the National Academy of Sciences of the United States of America96(16)9118-9123(1999) 2.Smith, C.A., Colvin, M., Storms, R.W., et al.BODIPY aminoacetaldehyde diethyl acetal08010501.81-15(2010) 3.Leng, Z., Yang, Z., Li, L., et al.A reliable method for the sorting and identification of ALDHhigh cancer stem cells by flow cytometryExp. Ther. Med.(2017) 4.Pomper, M.G., Wang, H., Minn, I., et al.Red fluorescent aldehyde dehydrogenase (ALDH) substrate(2015)

ALDH1A1-IN-4 (compound A1) functions as a powerful inhibitor of aldehyde dehydrogenase (ALDH) A1, exhibiting an IC 50 value of 0.32 μM. This compound is significant in cancer research [1].

Aldehyde dehydrogenase NAD(P) (ALDH) is an enzyme that facilitates the conversion of aldehydes into their respective carboxylic acids while simultaneously reducing the cofactor NAD(P) to NAD(P)H, making it a key component in biochemical research. This enzyme plays a crucial role in mitigating aldehyde stress by being part of the body's array of enzymatic defenses [1].

CM10 is an aldehyde dehydrogenase 1A family(ALDH1A) inhibitor.

NCT-505 is a potent and selective inhibitor of aldehyde dehydrogenase (ALDH1A1, IC50 = 7 nM) and a weak inhibitor of hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 with IC50 values of >57 μM, 22.8 μM, 20.1 μM, and >57 μM, respectively.

DOPAL is an aldehyde product of the oxidative deamination of dopamine by monoamine oxidase.[1] It can be further oxidized to 3,4-dihydroxyphenylacetic acid (DOPAC) by aldehyde dehydrogenase (ALDH) and, to a lesser extent reduced to 3,4-dihydroxyphenyl ethanol (DOPET). DOPAL is toxic to neurons.[2],[3] It can also oligomerize and precipitate α-synuclein, an event associated with Parkinson's disease.[2] Mice lacking cytosolic and mitochondrial forms of ALDH display increased levels of DOPAL as well as neurodegeneration and motor dysfunction characteristic of Parkinson's disease.[4]

4-Hydroxynonenal (4-HNE) (4-HNE) is an oxidative nitrosative stress biomarker. It is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2).

NCT-501 hydrochloride is a highly potent and selective inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), which is based on theophylline. It effectively inhibits hALDH1A1 with an IC50 value of 40 nM, exhibiting superior selectivity towards hALDH1A1 compared to other ALDH isozymes and dehydrogenases such as hALDH1B1, hALDH3A1, and hALDH2 (with IC50 values exceeding 57 μM).

11-Dehydro-2,3-dinor Thromboxane B2 (11-dehydro-2,3-dinor TXB2) is a metabolite derived from the inactive TXA2 metabolite, TXB2. Its formation involves the action of cytosolic aldehyde dehydrogenase (ALDH) and β-oxidation processes. Remarkably, levels of 11-dehydro-2,3-dinor TXB2 have been observed to increase by 5.2-fold in a surgery-induced rat model of tendon overuse, highlighting its potential role in physiological stress responses.

Methyl diethyldithiocarbamate is an active metabolite of the aldehyde dehydrogenase inhibitor disulfiram .1It is produced by methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes.2Methyl diethyldithiocarbamate inhibits liver low Kmaldehyde dehydrogenase (ALDH) in rats (ID50= 15.5 mg/kg).1It decreases mean arterial pressure (MAP) and increases heart rate during ethanol challenge in rats when administered at a dose of 20.6 mg/kg. 1.Hart, B.W., Yourick, J.J., and Faiman, M.D.S-methyl-N,N-diethylthiolcarbamate: A disulfiram metabolite and potent rat liver mitochondrial low Km aldehyde dehydrogenase inhibitorAlcohol7(2)165-169(1990) 2.Gessner, T., and Jakubowski, M.Diethyldithiocarbamic acid methyl ester. A metabolite of disulfiramBiochem. Pharmacol.21(2)219-230(1972)

Nitrefazole, a 4-nitroimidazole derivative, exhibits potent and prolonged inhibition of aldehyde dehydrogenase (ALDH), an enzyme critical for alcohol metabolism.

CVT-10216 is a Potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2) (IC50: 29 nM). CVT-10216 also has inhibitory effect of ALDH-1 (IC50: 1.3 μM). CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.

Alda-1 is an ALDH2 agonist, a cell-permeable activator of both the wild-type ALDH2*1 and the Asian E487K mutant ALDH2*2 forms of mitochondrial aldehyde dehydrogenase 2 (mtALDH2).